CAS: 22179-86-8; N-Hydroxy-4-(Trifluoromethyl)Benzenecarboximidamide

相似化合物

72111-09-2 40067-80-9 19227-13-5

上下游产品

CAS号455-18-5 对三氟甲基苯腈 | CAS号38980-96-0 4-三氟甲基苯脒盐酸盐 | CAS号131472-28-1 4-三氟甲基苯甲脒 | CAS号435303-34-7 5-氯甲基-3-(4-三氟甲基... | CAS号480390-86-1 4-(3-(4-(三氟甲基)苯...

📜对三氟甲基苯腈置于盐酸羟胺,三乙胺体系中,用 乙醇 用作溶剂,化学反应 4.0H,反应生成4-(三氟甲基)苄胺肟
参考文献:恶二唑酮使能的氮杂芳族伯胺的合成
标题:恶二唑酮使能的氮杂芳族伯胺的合成
摘要:尽管它们具有巨大的合成和制药用途,但基于普遍适用的c-h官能化策略,氮杂芳族伯胺仍然难以获得.恶二唑酮使能的方法据报道可方便地通过炔烃通过co(III)催化的氧化还原中性,阶跃,原子和纯化经济的chh功能化进入n-未取代的1-氨基异喹啉.甲15 ñ标记实验揭示了两个恶二唑酮n原子作为引导位点的有效性.可以将已安装的伯胺用作合成有用的手柄,用于附接发散的附件.
Doi:10.1021/acs.Orglett.6B02814

专利信息

专利号:US-9878999-B2
优先权日:2011-03-24
标题 :Proteasome chymotrypsin-like inhibition using PI-1833 analogs
发明人：LAWRENCE HARSHANI R; SEBTI SAID M; OZCAN SEVIL
权利人:H LEE MOFFITT CANCER CT & RES
摘要:Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).